Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00384

Target Information
NameEnoyl-[acyl-carrier-protein] reductase [NADH]    
Type of targetSuccessful target    
SynonymsInhA    
NADH-dependent enoyl-ACP reductase    
DiseaseTuberculosis
[ICD9: 010-018   ICD10: A15-A19]
[1][2]
Drug(s)EthionamideApprovedTuberculosis[3][4]
IsoniazidApprovedTuberculosis[5][6][7]
ProthionamideApprovedTuberculosis[3][8]
EC NumberEC 1.3.1.9
UniProt IDP0A5Y6
P46533
PDB Structure1BVR; 1ENY; 1ENZ; 1P44; 1P45; 1ZID; 2AQ8; 2AQH.    
FunctionInvolved in the resistance against the antituberculosis drugs isoniazid and ethionamide.    
SequenceMTGLLDGKRILVSGIITDSSIAFHIARVAQEQGAQLVLTGFDRLRLIQRITDRLPAKAPL LELDVQNEEHLASLAGRVTEAIGAGNKLDGVVHSIGFMPQTGMGINPFFDAPYADVSKGI HISAYSYASMAKALLPIMNPGGSIVGMDFDPSRAMPAYNWMTVAKSALESVNRFVAREAG KYGVRSNLVAAGPIRTLAMSAIVGGALGEEAGAQIQLLEEGWDQRAPIGWNMKDATPVAK TVCALLSDWLPATTGDIIYADGGAHTQLL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (4-benzylpiperidin-1-yl)[9]
(4-benzylpiperidin-1-yl)[9]
(4-benzylpiperidin-1-yl)[9]
(4-benzylpiperidin-1-yl)[9]
(4-phenylpiperazin-1-yl)[9]
2- (2-aminophenoxy)-5-hexylphenol[10]
2- (3-aminophenoxy)-5-hexylphenol[10]
2- (4,6-dimethoxypyrimidin-2-yloxy)-5-hexylphenol[10]
2- (4-aminophenoxy)-5-hexylphenol[10]
2- (4-hexyl-2-methoxyphenoxy)pyrimidine[10]
2-Hexadecynoic acid[11]
2-bromo-4-methylphenyl 2-nitrobenzoate[12]
2-nitro-N- (2,4,5-trichlorophenyl)benzamide[12]
4- (2-Thienyl)-1-[13]
4-chloro-N- (2,5-dichlorophenyl)-3-nitrobenzamide[12]
5-PENTYL-2-PHENOXYPHENOL[14]
5-hexyl-2- (2-nitrophenoxy)phenol[10]
5-hexyl-2- (3-nitrophenoxy)phenol[10]
5-hexyl-2- (4-nitrophenoxy)phenol[10]
5-hexyl-2- (pyrazin-2-yloxy)phenol[10]
5-hexyl-2- (pyridin-2-yloxy)phenol[10]
5-hexyl-2- (pyridin-3-yloxy)phenol[10]
5-hexyl-2- (pyridin-4-yloxy)phenol[10]
5-hexyl-2- (pyrimidin-2-yloxy)phenol[10]
5-hexyl-2-phenoxyphenol[10]
5-octyl-2-phenoxyphenol[15]
Beta-D-Glucose[13]
C16-Fatty-Acyl-Substrate-Mimic[13]
Diclosan[13]
Ethionamide[3][4]
Genz-10850[13]
Indole Naphthyridinone[13]
Isoniazid[5][6][7]
N- (2,4-dichlorophenyl)-2-nitrobenzamide[12]
N- (2,4-dichlorophenyl)-4-methyl-3-nitrobenzamide[12]
N- (2,4-dimethylphenyl)-2-nitrobenzamide[12]
N- (2,5-dichlorophenyl)-4-methoxy-3-nitrobenzamide[12]
N- (2-[10]
N- (3,5-dichlorophenyl)-2-nitrobenzamide[12]
N- (3,5-dichlorophenyl)-4-methoxy-3-nitrobenzamide[12]
N- (3,5-dimethoxyphenyl)-4-methyl-2-nitrobenzamide[12]
N- (3-[10]
N- (4-[10]
N- (4-[12]
N- (4-METHYLBENZOYL)-4-BENZYLPIPERIDINE[14]
Nicotinamide-Adenine-Dinucleotide[13]
Prothionamide[3][8]
TRICLOSAN[14]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Inhibition of InhA activity, but not KasA activity, induces formation of a KasA-containing complex in mycobacteria. J Biol Chem. 2003 Jun 6;278(23):20547-54. Epub 2003 Mar 24. To Reference
Ref 2Overexpression of inhA, but not kasA, confers resistance to isoniazid and ethionamide in Mycobacterium smegmatis, M. bovis BCG and M. tuberculosis. Mol Microbiol. 2002 Oct;46(2):453-66. To Reference
Ref 3Mechanism of thioamide drug action against tuberculosis and leprosy. J Exp Med. 2007 Jan 22;204(1):73-8. Epub 2007 Jan 16. To Reference
Ref 4Calcium-activated conductance in skate electroreceptors: current clamp experiments. J Gen Physiol. 1977 Feb;69(2):121-43. To Reference
Ref 5Diversity in enoyl-acyl carrier protein reductases. Cell Mol Life Sci. 2009 May;66(9):1507-17. To Reference
Ref 6Enoyl reductases as targets for the development of anti-tubercular and anti-malarial agents. Curr Drug Targets. 2007 Mar;8(3):399-411. To Reference
Ref 7Screening for novel antituberculosis agents that are effective against multidrug resistant tuberculosis. Curr Top Med Chem. 2007;7(5):499-507. To Reference
Ref 8Ability of the Ca2+ ionophores A23187 and ionomycin to mimic some of the effects of the tumor promoter 12-O-tetradecanoylphorbol-13-acetate on hydroperoxide production, ornithine decarboxylase activity, and DNA synthesis in mouse epidermis in vivo. Cancer Res. 1990 Sep 15;50(18):5806-12. To Reference
Ref 9Bioorg Med Chem. 2007 Nov 1;15(21):6649-58. Epub 2007 Aug 15.Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides. To Reference
Ref 10Bioorg Med Chem Lett. 2008 May 15;18(10):3029-33. Epub 2008 Apr 18.Synthesis and in vitro antimycobacterial activity of B-ring modified diaryl ether InhA inhibitors. To Reference
Ref 11Bioorg Med Chem. 2010 Nov 1;18(21):7475-85. Epub 2010 Sep 18.2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. To Reference
Ref 12Eur J Med Chem. 2009 Sep;44(9):3718-30. Epub 2009 Apr 8.Discovery of potential new InhA direct inhibitors based on pharmacophore and 3D-QSAR analysis followed by in silico screening. To Reference
Ref 13Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 14Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 15J Med Chem. 2008 May 8;51(9):2606-12. Epub 2008 Apr 5.Natural products, small molecules, and genetics in tuberculosis drug development. To Reference



 

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